DNA binding cationic bolasomes with delocalized charge center : A structure-activity relationship study

作者: C. Lizano , V. P. Torchilin , V. Weissig , C. R. Ganellin

DOI:

关键词: Structure–activity relationshipStereochemistryCationic polymerizationVesicleDelocalized electronBolaamphiphileChemistryDNAA-DNARing (chemistry)

摘要: Bolaamphiphilic dicationic quinolinium derivatives are being explored by us for the development of mitochondria-specific drug and DNA delivery systems. In this structure-activity relationship study, defined connections between structure bolaamphiphiles their ability to form cationic vesicles (bolasomes) bind established. Nine with varying polar head groups hydrophobic tail segments were synthesized according published procedures. Their self-assembly behavior was determined photon correlation spectroscopy affinity measured using fluorescence dye SYBR Green I. The introduction a binding capacity allows quantitative comparison Lipofectin regarding lipoplexes. It is demonstrated that primary 4-amino group at ring system plays an important role in binding. presence bulky aliphatic residue aromatic favors these into bolasomes.

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